Rj. Booth et Jc. Hodges, POLYMER-SUPPORTED QUENCHING REAGENTS FOR PARALLEL PURIFICATION, Journal of the American Chemical Society, 119(21), 1997, pp. 4882-4886
The preparation of polystyrene-divinylbenzene-supported derivatives of
tris(2-aminoethyl)amine and methyl isocyanate are described. These po
lymeric reagents are used to quench excess reactants and remove known
impurities from the crude reaction products obtained from the solution
-phase, parallel syntheses of ureas, thioureas, sulfonamides, amides,
and pyrazoles. In conjunction with the use of other polymeric reactant
s during the course of a reaction, the addition of polymer-supported q
uench reagent(s) at the conclusion of the reaction allows isolation of
the desired product by a single filtration and evaporation of solvent
. The mechanical simplicity and efficiency of this methodology make po
ssible the rapid, parallel purification of crude reaction products obt
ained via solution-phase syntheses, regardless of whether the intended
product is a single compound or a mixture of compounds, and hence off
ers an attractive alternative to solid-phase organic synthesis in the
practice of combinatorial chemistry.